Clidiniumbromid

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

• Sicherheit

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P270：Bei Gebrauch nicht essen, trinken oder rauchen.

  P301+P312：BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Clidinium bromide Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R22:Gesundheitsschädlich beim Verschlucken.

• S-Sätze Betriebsanweisung:

  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

• Beschreibung

  Clidinium is a gastrointestinal muscarinic receptor antagonist (K_i = 3 nM against [³H]quinuclidinyl benzilate binding in rat colonic enterocytes). Administration of clidinium, at a dose of 1 mg/kg, slows intestinal transit and induces constipation in mice. This clidinium-induced constipation induces serum hyperammonemia and decreases clonic, myoclonic, and tonic seizure thresholds in a murine pentylenetetrazole-induced epilepsy model.

• Chemische Eigenschaften

  White Crystalline Solid

• Originator

  Librax,Roche,US,1961

• Verwenden

  An anticholinergic. Used as an antispasmodic.

• Verwenden

  Clidinium inhibits muscarinic action of acetylcholine on postganglionic parasympathetic effector regions. It is used for treating stomach ulcers.

• Definition

  ChEBI: The bromide salt of clinidium. It is used for the symptomatic treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome.

• Manufacturing Process

  5.12 g of 1-azabicyclo[2.2.2]-3-octanol were refluxed with a suspension of 0.92 g of finely divided sodium in 50 cc of toluene, until most of the sodium had reacted (about 4 hours). The thus obtained suspension of the white amorphous alcoholate was cooled with ice, and reacted with 10.16 g of diphenylchloroacetyl chloride, which was added in form of a solution in approximately 40 cc of toluene. The mixture was stirred for 1 hour at room temperature. Small amounts of unreacted sodium were destroyed with isopropanol, and 120 cc of 1 N hydrochloric acid were then added, The mixture was refluxed for 1/2 hour, in order to convert the first formed product, diphenylchloroacetic acid ester of 1-azabicyclo[2.2.2]-3-octanol, into the corresponding benzilic acid ester.
  The toluene phase was separated and discarded. The aqueous phase, together with a precipitated water- and toluene-insoluble oil, was made alkaline and extracted repeatedly with chloroform. The chloroform solution was concentrated in vacuo. The residue was recrystallized from a mixture of acetone and ether (alternatively, from chloroform and ether), and formed needles melting at 164° to 165°C. It was identified as 3-benziloyloxy-1- azabicyclo[2.2.2]octane.
  3-Benziloyloxy-1-azabicyclo[2.2.2]octane methobromide was prepared by adding 20 cc of a 30% solution of methyl bromide in ether to a solution of 2.5 g of 3-benziloyloxy-1-azabicyclo[2.2.2]octane in 20 cc of chloroform. After standing for 3 hours at room temperature and 15 hours at +5°C, a crystalline precipitate had formed. This was filtered off and recrystallized from a mixture of methanol, acetone, and ether; prisms melting at 240° to 241°C.

• Trademarks

  Quarzan (Roche).

• Therapeutic Function

  Anticholinergic, Antiulcer

• Allgemeine Beschreibung

  Clidinium bromide, 3-hydroxy-1-methylquinuclidinium bromide benzilate (Quarzan),is a white or nearly white, almost odorless, crystalline powderthat is optically inactive. It is soluble in water and alcohol butonly very slightly soluble in ether and benzene.

• Clinical Use

  This anticholinergic agent is marketed alone and in combinationwith the minor tranquilizer chlordiazepoxide (Librium)in a product known as Librax. The rationale of the combinationfor the treatment of GI complaints is the use of an anxiety-reducing agent together with an anticholinergic agent,based on the recognized contribution of anxiety to the developmentof the diseased condition. It is suggested for pepticulcer, hyperchlorhydria, ulcerative or spastic colon, anxietystates with GI manifestations, nervous stomach, irritable orspastic colon, and others. Clidinium bromide is contraindicatedin glaucoma and other conditions that may be aggravatedby the parasympatholytic action, such as prostatic hypertrophyin elderly men, which could lead to urinary retention.

• Synthese

  Clidinium, 3-benzyloyloxy-1-methylcynuclidinium bromide (14.1.19), is synthesized by reacting 3-hydroxycynuclidine (14.1.17) with the of benzilic acid chloride producing the ester (14.1.18), which if further alkylated at the nitrogen atom by methylbromide, giving clidinium (14.1.19) [16].

  

Clidinium bromide Upstream-Materialien And Downstream Produkte

Clidiniumbromid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(120)Suppliers

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